1357389-11-7
基本信息
(2E)-N-(2-氨基-4-氟苯基)-3-[1-(3-苯基-2-丙烯-1-基)-1H-吡唑-4-基]-2-丙烯酰胺
RGFP966
RGFP-966
RGFP 966
(E/Z)-RGFP 966
RGFP966, >=98%
RGFP966
RGFP-966
(2E)-N-(2-Amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-2-propenamide
2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-(3-phenyl-2-propen-1-yl)-1H-pyrazol-4-yl]-, (2E)-
物理化学性质
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2024/08/19 | HY-13909 | RGFP966 RGFP966 | 1357389-11-7 | 5mg | 900元 |
2024/08/19 | HY-13909 | RGFP966 RGFP966 | 1357389-11-7 | 10mM * 1mLin DMSO | 990元 |
2024/08/19 | HY-13909 | RGFP966 RGFP966 | 1357389-11-7 | 10mg | 1183元 |
常见问题列表
HDAC3 80 nM (IC 50 ) |
RGFP966 potently and selectively inhibits HDAC 3 with IC 50 of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC 50 =5.6 μM), 2 (9.7 μM) and 8 (>100 μM), indicating a good level of selectivity for HDAC 3. The mRNA levels of HDACs 1, 2 and 3 are not significantly affected by RGFP966 in RAW 264.7 macrophages, whereas the HDAC 1 and HDAC 2 protein levels are slightly, though significantly, reduced upon RGFP966 treatment. Moreover, RGFP966 significantly reduced the transcriptional activity of NF-κB p65, whereas NF-κB p65 acetylation and localization remain unaltered.
RGFP966 (10 and 25 mg/kg) treatment significantly improves body weight, rotarod performance and several measures of motor function in the open field locomoter test. RGFP966 at a 10 mg/kg dose penetrates the blood-brain barrier into rat auditory cortex with typical pharmacokinetics, which together establish feasibility for the modulation of A1 plasticity due to action in the auditory cortex.